Catalytic Asymmetric Biginelli Reaction for the Enantioselective Synthesis of 3,4- Dihydropyrimidinones (DHPMs)

Author(s): Jie-Ping Wan, Yunfang Lin, Yunyun Liu.

Journal Name: Current Organic Chemistry

Volume 18 , Issue 6 , 2014

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Graphical Abstract:


Biginelli reaction is the most classical and frequently employed method for facile and diverse synthesis of 3,4- dihydropyrimidinones and thiones (DHPMs)-a class of privileged heterocyclic scaffolds possessing meritorious biological and pharmacological functions. Owing to the presence of a chiral centre in DHPMs and the discovered distinction in biological activity of DHPMs isomers, accessing chiral DHPMs of optical purity constitutes a core issue of particular importance in the research of Biginelli reaction. Following the rapid progress of modern organic synthesis, catalytic asymmetric Biginelli reaction has gradually evolved as the mainstream method instead of early kinetic resolution for acquiring enantiomerically enriched. In the present paper, the advances in catalytic asymmetric Biginelli reaction, including advances in metal catalysis as well as organocatalysis, are comprehensively reviewed.

Keywords: Asymmetric, Biginelli reaction, catalytic, DHPMs, enantioselective.

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Article Details

Year: 2014
Page: [687 - 699]
Pages: 13
DOI: 10.2174/138527281806140415235855
Price: $58

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